C-2位硫桥式四环氟喹诺酮抗菌素W1的合成与抗菌活性

Synthesis and Antibacterial Activity of C-2 Sulfur-Bridged Tetracyclofluoroqui nolone Antibacterial Agent W1

合成了一个新的 C-2位硫桥式四环氟喹诺酮抗菌素 7-氟 -8-[(1 S,4 S) -5 -甲基 -2 ,5 -二氮杂双环 [2 .2 .1 ]庚烷 -2 ]-9,1 -(环氧亚甲基 ) -5 -氧 -5 H噻唑并 [3 ,2 -a]喹啉 -4 -羧酸盐酸盐 (W1 ) ,未见文献报道。W1经元素分析、红外光谱、核磁共振光谱作了结构鉴定 ,并通过两倍琼脂稀释法对其 MICs进行了测定 ,以氧氟沙星作对照 ,结果表明 :W1显示极好的抗菌活性 ,其抗 G+菌 (包括耐甲氧西林的金黄色葡萄球菌 )的活性比氧氟沙星至少强4倍 ,抗 G- 菌 (包括绿脓杆菌 )

A new C-2 sulfur-bridged tetracyclofluoroquinolone antibacte ri al agent 7-fluoro-8-[(\%1S,4S\%)-5-methyl-2,5-diazabicyclo[2.2.1]he ptyl -2]-9,1-(epoxymethano)-5-oxo-5H-thiazolo-9,1-(epoxymethano)-5-oxo-5H-thiazoloquinoline-4-carb o xylic acid hydrochloride(W1)was prepared which was not reported previously.W1 was identified by elemental analysis,IR,1HNMR and MS.The MICs of W1 was defermine d according to the standard method by a serial 2-fold agar dilution technique w ith ofloxacin for comparison.W1 exhibited excellent activity with at least 4-fo ld more potent than ofloxacin against Gram-posifive bacteria including methici llin-resistant, \%Staphylococcus aureus\% and at least 2-fold more potent than ofloxacin against Gram-negative bacteria including \%Pseudomonas aeruginosa\%.